Colin J N, Singlas E
Ann Fr Anesth Reanim. 1985;4(6):465-70. doi: 10.1016/S0750-7658(85)80242-2.
Atracurium is a new neuromuscular blocking agent which has an unique mode of elimination by spontaneous degradation in slightly alkali solution, according to the Hofmann elimination. The Hofmann elimination is completed in plasma (in vitro or in vivo) by an ester hydrolysis. The major degradation product is laudanosine. Metabolites can be considered as pharmacologically inactive with the usual doses of atracurium. Spontaneous degradation of atracurium in plasma is the major route of elimination in man and contributes to a short elimination half-life (approximatively 20 min). Distribution half-life is short and central and peripheral volumes are small when compared with the usual neuromuscular blocking agents. The pharmacokinetic parameters give a rapid dynamic equilibrium so that incremental doses will not lead to accumulation phenomenon. Because of spontaneous degradation of atracurium in plasma, its kinetics are theoretically independent of renal and liver functions. Only a slight increase of distribution volumes can be seen in very severe renal/hepatic failure. Atracurium pharmacokinetics could theoretically be modified by some modifications of acid-base equilibrium or alterations of thermoregulation. Pharmacokinetic studies are not yet available in these areas.
阿曲库铵是一种新型神经肌肉阻滞剂，根据霍夫曼消除反应，它在弱碱性溶液中通过自发降解有一种独特的消除方式。霍夫曼消除反应在血浆中（体外或体内）通过酯水解完成。主要降解产物是劳丹诺辛。在常用剂量的阿曲库铵下，代谢产物可被认为无药理活性。阿曲库铵在血浆中的自发降解是人体消除的主要途径，这导致其消除半衰期较短（约20分钟）。与常用的神经肌肉阻滞剂相比，其分布半衰期较短，中央和外周容积较小。药代动力学参数能快速达到动态平衡，因此追加剂量不会导致蓄积现象。由于阿曲库铵在血浆中的自发降解，其动力学理论上与肾和肝功能无关。在非常严重的肾/肝功能衰竭时，仅可见分布容积略有增加。理论上，酸碱平衡的某些改变或体温调节的改变可能会改变阿曲库铵的药代动力学。目前这些领域尚无药代动力学研究。
